Triapine (3-AP) |
Katalog-Nr.GC17897
One-Click Copy Product Info
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Triapine (3-AP) is a ribonucleotide reductase (RNR) M2 subunit inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 143621-35-6
Sample solution is provided at 25 µL, 10mM.
Triapine (3-AP) is a ribonucleotide reductase (RNR) M2 subunit inhibitor. Triapine forms a chelator with intracellular iron ions. Triapine can be used in research related to cervical cancer, pancreatic cancer, leukemia, and glioma[1-4].
In vitro, pretreatment of Ewing sarcoma cells (WE-68, SK-ES-1, A673) with VE821 (1-5μM) for 1 hour, followed by treatment with Triapine (0.125–1μM) for 48 hours. Triapine significantly synergistically induced cell death, while promoting mitochondrial membrane potential dissipation and caspase 3/7 activity[5]. Treatment of SKOV-3-DR-GFP cells with Triapine (0.75μM) for 24-48 hours. Triapine significantly inhibited homologous recombination repair activity[6].
In vivo, Triapine (10mg/kg; administered for 5 consecutive days per week) was intraperitoneally injected into female athymic nude mice bearing SKOV-3 tumors for 4 weeks. Triapine alone had minimal effect on tumor growth delay, but significantly enhanced tumor growth delay when combined with carboplatin and liposomal doxorubicin[7]. Triapine (10mg/kg; administered for 5 consecutive days per week) combined with olaparib (50mg/kg) and cediranib (0.75mg/kg) was intraperitoneally injected into female athymic nude mice bearing SKOV3 or OVCAR3 tumors for 6 weeks. The combination of Triapine, olaparib, and cediranib significantly suppressed the growth of BRCA-wild type epithelial ovarian cancer and prolonged the survival of mice[8].
References:
[1] Martin LK, Grecula J, Jia G, et al. A dose escalation and pharmacodynamic study of triapine and radiation in patients with locally advanced pancreas cancer. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e475-81.
[2] Yalowich JC, Wu X, Zhang R, et al. The anticancer thiosemicarbazones Dp44mT and triapine lack inhibitory effects as catalytic inhibitors or poisons of DNA topoisomerase IIα. Biochem Pharmacol. 2012 Jul 1;84(1):52-8.
[3] Whitnall M, Howard J, Ponka P, et al. A class of iron chelators with a wide spectrum of potent antitumor activity that overcomes resistance to chemotherapeutics. Proc Natl Acad Sci U S A. 2006 Oct 3;103(40):14901-6.
[4] Qu Q, Chen Y, Wang Y, et al. Lithocholic acid phenocopies anti-ageing effects of calorie restriction. Nature. 2025 Jul;643(8070):192-200.
[5] Sturm MJ, Henao-Restrepo JA, Becker S, et al. Synergistic anticancer activity of combined ATR and ribonucleotide reductase inhibition in Ewing's sarcoma cells. J Cancer Res Clin Oncol. 2023 Sep;149(11):8605-8617.
[6] Lin ZP, Ratner ES, Whicker ME, et al. Triapine disrupts CtIP-mediated homologous recombination repair and sensitizes ovarian cancer cells to PARP and topoisomerase inhibitors. Mol Cancer Res. 2014 Mar;12(3):381-393.
[7] Ratner ES, Zhu YL, Penketh PG, et al. Triapine potentiates platinum-based combination therapy by disruption of homologous recombination repair. Br J Cancer. 2016 Mar 29;114(7):777-86.
[8] Lin ZP, Zhu YL, Lo YC, et al. Combination of triapine, olaparib, and cediranib suppresses progression of BRCA-wild type and PARP inhibitor-resistant epithelial ovarian cancer. PLoS One. 2018 Nov 16;13(11):e0207399.
| Cell experiment [1]: | |
Cell lines | SKOV-3-DR-GFP cells (human ovarian cancer cell line) |
Preparation Method | SKOV-3-DR-GFP cells were treated with 0.75μM Triapine for 24 hours followed by an additional 24 hours of incubation treated continuously with 0.75μM Triapine for 48 hours. |
Reaction Conditions | 0.75μM; 24-48h pretreatment |
Applications | Triapine treatment for 24 hours followed by 24-hour recovery resulted in more than a 50% decrease in I-SceI-induced homologous recombination repair (HRR) activity. Continuous treatment with Triapine for 48 hours led to nearly complete abrogation of I-SceI-induced HRR activity. |
| Animal experiment [2]: | |
Animal models | Athymic nude mice and SCID-Beige mice |
Preparation Method | For subcutaneous xenograft experiments, SKOV3 or OVCAR3 cells suspended in serum-free medium mixed with Matrigel were implanted subcutaneously. For intraperitoneal xenograft experiments, PEO4ip cells suspended in serum-free medium were implanted intraperitoneally. Mice were treated intraperitoneally with vehicle or Triapine+olaparib+cediranib once daily for 5 consecutive days per week. |
Dosage form | 10mg/kg; i.p.; daily for 5 consecutive days per week for 6 weeks |
Applications | Triapine alone had no inhibitory effects on the growth of SKOV3 xenografts in mice. The combination of Triapine, olaparib, and cediranib resulted in marked suppression of BRCA-wild type epithelial ovarian cancer growth and significant prolongation of the survival time of mice in both subcutaneous and intraperitoneal xenograft models. |
References: | |
| Cas No. | 143621-35-6 | SDF | |
| Chemical Name | [(E)-(3-aminopyridin-2-yl)methylideneamino]thiourea | ||
| Canonical SMILES | C1=CC(=C(N=C1)C=NNC(=S)N)N | ||
| Formula | C7H9N5S | M.Wt | 195.24 |
| Löslichkeit | ≥ 83.3mg/mL in DMSO | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.1219 mL | 25.6095 mL | 51.219 mL |
| 5 mM | 1.0244 mL | 5.1219 mL | 10.2438 mL |
| 10 mM | 512.2 μL | 2.561 mL | 5.1219 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)